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Licogliflozin

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Chemical Structure| 1291094-73-9 同义名 : LIK066
CAS号 : 1291094-73-9
货号 : A237947
分子式 : C23H28O7
纯度 : 98%+
分子量 : 416.464
MDL号 : MFCD31630771
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(252.12 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 2 mg/mL(4.8 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 The sodium-glucose co-transporters (SGLTs) 1 and 2 play an important role in glucose and sodium transport in the kidneys and gastrointestinal tract. SGLT1 is expressed in the small intestine, where is needed for glucose and galactose absorption. Inhibition of SGLT1 results in glucose and galactose malabsorption[1]. Licogliflozin is a combined inhibitor of SGLT1 and SGLT2 and is hypothesized to further enhance the effects on renal sodium and glucose handling via inhibition of both cotransporter subtypes in the proximal renal tubule. Licogliflozin demonstrated significant weight loss (~6%) versus placebo, with favorable changes in metabolic parameters and incretin hormones. Dual inhibition of SGLT1/2 with licogliflozin in the gut and kidneys is an attractive strategy for treating obesity and diabetes[2]. Oral absorption of licogliflozin was rapid (tmax < 1 h) with absorption estimated at 87%, 100% and 77% in rats, dogs and humans, respectively. Excretion of licogliflozin-related radioactivity was rapid and nearly complete following oral administration with total radioactivity recovery ranging from 73% in dogs, 92.5% in humans, to 100% in rats. Elimination of licogliflozin was predominantly via metabolism with the majority of the radioactivity dose (∼54-74%) excreted as metabolites across species[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.01mL

2.40mL

1.20mL

24.01mL

4.80mL

2.40mL
参考文献

[1]Turk, E., et al. Glucose/galactose malabsorption caused by a defect in the Naþ/glucose cotransporter. Nature. 1991. 350 (6316), 354–356.

[2]He YL, Haynes W, et al. The effects of licogliflozin, a dual SGLT1/2 inhibitor, on body weight in obese patients with or without diabetes. Diabetes Obes Metab. 2019. 21(6), 1311-1321.

[3]Lydia Wang-Lakshman,et al. Pharmacokinetics, metabolism, and excretion of licogliflozin, a dual inhibitor of SGLT1/2, in rats, dogs, and humans. Xenobiotica. 2021. 51(4), 413-426.